L-脯氨酰-L-亮氨酰-甘氨酸酰胺对大鼠阿扑吗啡作用的增强作用。

Potentiation of apomorphine action in rats by l-prolyl-l-leucyl-glycine amide.

作者信息

Kostrzewa R M, Kastin A J, Sobrian S K

出版信息

Pharmacol Biochem Behav. 1978 Sep;9(3):375-8. doi: 10.1016/0091-3057(78)90299-x.

Abstract

Although the antiparkinsonian activity of 1-prolyl-l-leucyl-glycine amide (PLG=MIF-I) has been previously observed in several clinical trials, little is known of the mechanism of action of this tripeptide on the brain. Our study demonstrated potentiation of the action of apomorphine by PLG on the rotational behavior of mature rats which received unilateral 6-OHDA (16 microgram) lesions of the striatum as neonates. No change in tyrosine hydroxylase or dopa decarboxylase activities in rat striatal homogenates was found after addition of PLG (10(-8-10(-3) M). The results suggest that PLG modifies the dopamine receptor, making it more responsive to stimulation by the agonistic agent apomorphine and perhaps by the natural neurotransmitter dopamine.

摘要

尽管此前在多项临床试验中已观察到1-脯氨酰-L-亮氨酰-甘氨酸酰胺（PLG = MIF-I）的抗帕金森病活性，但对于这种三肽在大脑中的作用机制却知之甚少。我们的研究表明，PLG可增强阿扑吗啡对成熟大鼠旋转行为的作用，这些大鼠在新生时接受了单侧纹状体6-羟基多巴胺（16微克）损伤。加入PLG（10^(-8) - 10^(-3) M）后，大鼠纹状体匀浆中的酪氨酸羟化酶或多巴脱羧酶活性未发生变化。结果表明，PLG可修饰多巴胺受体，使其对激动剂阿扑吗啡以及可能对天然神经递质多巴胺的刺激更敏感。